Gefapixant

Gefapixant is an allosteric antagonist of the purinergic P2X3 receptor. It inhibits agonist-induced P2X3 and P2X2/3 currents in 1321N1 cells co-expressing human P2X2 and P2X3 (IC50s = 153 and 220 nM, respectively) but does not inhibit P2X2 currents in the same cells at 10 µM. In vivo, gefapixant (30 mg/kg) increases the paw withdrawal threshold and decreases weight-bearing discomfort in a rat model of inflammatory hyperalgesia induced by complete Freund's adjuvant (CFA) and a rat model of neuropathic pain induced by sciatic nerve injury. Gefapixant (10 mg/kg) improves cardiac function, reduces cardiac TNF-alpha levels, and prevents cardiac fibrosis in a rat model of myocardial infarction induced by left anterior descending (LAD) branch ligation. Formulations containing gefapixant have been used in the treatment of chronic cough.Formal Name: 5-[(2,4-diamino-5-pyrimidinyl)oxy]-2-methoxy-4-(1-methylethyl)-benzenesulfonamide. CAS Number: 1015787-98-0. Synonyms: AF-219, MK-7264, Ro 4926219. Molecular Formula: C14H19N5O4S. Formula Weight: 353.4. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Slightly soluble: 0.1-1 mg/ml. SMILES: O=S(N)(C1=C(OC)C=C(C(C)C)C(OC2=CN=C(N)N=C2N)=C1)=O. InChi Code: InChI=1S/C14H19N5O4S/c1-7(2)8-4-10(22-3)12(24(17,20)21)5-9(8)23-11-6-18-14(16)19-13(11)15/h4-7H,1-3H3,(H2,17,20,21)(H4,15,16,18,19). InChi Key: HLWURFKMDLAKOD-UHFFFAOYSA-N.